This invention relates to 3'-amino-2'halo-anthracycline anti-cancer antibiotics. The term antibiotic is used herein in its original sense to mean "a metabolic product of a microorganism or a derivative thereof" and does not necessarily imply that the compounds possess significant antibacterial activity.
Anthracyline antibiotics including doxorubicin, daunorubicin, and carminomycin have emerged as important chemotherapeutic agents in the treatment of a broad specturm of neoplastic conditions including acute myloblastic and lymphoplastic leukemias. Doxorubicin (also known as Adriamycin) is the subject of U.S. Pat. No. 3,590,028 and is a prescribed antineoplastic agent used in a number of chemotherapeutic treatments.
Certain undesirable side effects have limited the usefulness of know anthracycline antibiotics. One of their more serious side effects, however, is their cardiotoxicity which severly restricts the dosages and the frequency with which the antibiotic can be administered and, in turn, limits their overall effectiveness as an antibiotic. Many of the other side effects which accompany the administration of these agents can be managed by administering other pharmaceutical agents in combination with them; however, the cardiopathic effects are not easily controlled or reversed.
In view of the proven effectiveness of known anthracyclines in the treatment of cancer, efforts have been undertaken to develop less toxic derivatives which can be administered in high, more effective dosages with greater frequency. This invention seeks to provide such derivatives.